ZK 216348  (Synonyms: (+)-ZK 216348)

ZK 216348 ((+)-ZK 216348) is a nonsteroidal selective glucocorticoid receptor agonist with an IC₅₀ of 20.3 nM. ZK 216348 also binds to Progesterone and mineralocorticoid receptors with IC₅₀s of 20.4 nM and 79.9 nM, respectively. ZK 216348 has antiinflammatory activity similar to Prednisolone and induces less transactivation-mediated side effects^[1][2].

IC50: 20.3 nM (Glucocorticoid recepto), 20.4 nM (Progesterone receptor ) and 79.9 nM (mineralocorticoid receptor)^[1]

In human peripheral blood mononuclear cells (PBMCs), ZK 216348 inhibits TNF-α and IL-12 with IC₅₀ of 89 nM and 52 nM, respectively^[1].
Participation of an active GR in the antiinflammatory response of ZK 216348 is further investigated in Caco-2 cells, where the TNF-α-induced expression of the proinflammatory cytokine IL-8 is suppressed in the presence of ZK 216348^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ZK 216348 (1-30 mg/kg; subcutaneous injection; for 24 hours; NMRI mice and Wistar rats) treatment inhibits ear edema in both mice and rats. A markedly superior side-effect profile is found in ZK 216348 with regard to increases in blood glucose, spleen involution, and, to a lesser extent, skin atrophy^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

476.45

C₂₄H₂₃F₃N₂O₅

669073-68-1

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Schäcke H, et al. Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc Natl Acad Sci U S A. 2004 Jan 6;101(1):227-32.  [Content Brief]

  [2]. Reuter KC, et al. Selective glucocorticoid receptor agonists for the treatment of inflammatory bowel disease: studies in mice with acute trinitrobenzene sulfonic acid colitis. J Pharmacol Exp Ther. 2012 Apr;341(1):68-80.  [Content Brief]